38058-86-5Relevant articles and documents
EPIDITHIODIKETOPIPERAZINE COMPOUNDS, COMPOSITIONS, AND METHODS
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, (2015/07/07)
Epidithiodiketopiperazine compounds, pharmaceutical compositions based thereon and methods of their synthesis, as part of treating, inhibiting and reducing transcription and translation of hypoxia inducible genes are described. In another aspect, the present disclosure describes a method for interfering with hypoxia-induced transcriptional pathway in a cell comprising: contacting the cell with at least one compound disclosed herein. In another aspect, the present disclosure describes a method for treating breast cancer, a solid cancer, a blood cancer, a subject suffering from carcinoma in need of said treatment, and renal cell carcinoma (RCC), comprising: administering to the subject an effective amount of at least one compound disclosed herein. In some embodiments of the methods described herein, the method further comprises administering an additional anti-cancer and/or cytotoxic agent.
Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes
Taladriz, Andrea,Healy, Alan,Flores Pérez, Eddysson J.,Herrero García, Vanessa,Ríos Martínez, Carlos,Alkhaldi, Abdulsalam A. M.,Eze, Anthonius A.,Kaiser, Marcel,De Koning, Harry P.,Chana, Antonio,Dardonville, Christophe
, p. 2606 - 2622 (2012/06/01)
A series of 73 bisphosphonium salts and 10 monophosphonium salt derivatives were synthesized and tested in vitro against several wild type and resistant lines of Trypanosoma brucei (T. b. rhodesiense STIB900, T. b. brucei strain 427, TbAT1-KO, and TbB48). More than half of the compounds tested showed a submicromolar EC50 against these parasites. The compounds did not display any cross-resistance to existing diamidine therapies, such as pentamidine. In most cases, the compounds displayed a good selectivity index versus human cell lines. None of the known T. b. brucei drug transporters were required for trypanocidal activity, although some of the bisphosphonium compounds inhibited the low affinity pentamidine transporter. It was found that phosphonium drugs act slowly to clear a trypanosome population but that only a short exposure time is needed for irreversible damage to the cells. A comparative molecular field analysis model (CoMFA) was generated to gain insights into the SAR of this class of compounds, identifying key features for trypanocidal activity.
The 4,4′-(1,2-ethanediyl)bisbenzyl biradical: Its generation, detection, and (photo)chemical behavior in solution
Miranda,Font-Sanchis,Perez-Prieto,Scaiano
, p. 2717 - 2721 (2007/10/03)
The 4,4′-(1,2-ethanediyl)bisbenzyl biradical (2) is clearly and efficiently generated by photolysis of [3.2]paracyclophane-2-one (8) in cyclohexane solution. This intermediate is also formed via two-photon processes from [2.2]paracyclophane (3) and 1,2-bi
Reductive Coupling by Chromium(0) - (Bibenzyl)- and (Stilbene)tricarbonylchromium(0) Complexes by a One-Pot Reaction from Benzylic Halides
Wey, Hans G.,Butenschoen, Holger
, p. 93 - 99 (2007/10/02)
Reaction of Cr(CO)3(NH3)3 with benzylic mono-, di-, and trihalides leads to the formation of 1,2-diarylethanes, -ethenes, and diphenylethyne in satisfactory yields.Di(halomethyl)benzene derivatives yield product mixtures containing both reduction products and coupling products.With a higher excess in chromium(0), under otherwise unchanged reaction conditions, the corresponding (arene)tricarbonylchromium(0) complexes of the coupling products are formed in a one-pot reaction from the benzylic halides.